Lapatinib of formula-(1), is reported for the first time by M. C. Carter et.al in PCT International Publication No.: WO 99/35146 (1999 to Glaxo). Its equivalent US patent is U.S. Pat. No. 6,727,256 (2004 to SmithKline Beecham). Study on mechanism of action of Lapatinib is described in Oncogene, 21, 6255 (2002). In vitro anti-tumor activity in combination with anti-ErbB2 antibodies is described in Oncogene, 24, 6213 (2005), biological effects on tumor growth is described in J. Clin. Oncol, 23, 2502 (2005) and pharmacokinetics and clinical activity in metastatic carcinomas is described in J. clin. oncol, 23, 5305 (2005).
The process for the preparation of Lapatinib of formula-(1), disclosed in WO99/35146, is given in the Scheme-A. Accordingly, 4-chloro-6-iodo-quinazoline of formula-(2), is reacted with 3-chloro-4-(31-fluoro-benzyloxy)-aniline yielding N-[3-chloro-4-{(31-fluoro-benzyloxy)phenyl}]-6-iodo-quinazoline of formula-(3). The compound of the formula-(3) reacts with (1,3-dioxolan-2-yl)-2-(tributylstannyl)furan to get the compound of formula-(4a) which on reaction with HCl, removes the protecting group and liberates 5-(4-{3-chloro-4-(3-fluoro-benzyloxy)anilino}-6-quinazolinyl)-furan-2-carbaldehyde of formula-(4). The compound of the formula-(4) on reaction with 2-methanesulfonylethylamine, followed by reduction using sodium (triacetoxy)borohydride as the reducing agent gives the required compound Lapatinib of formula-(1) as an organic residue, which is purified by column chromatography. If desired the isolated material is then converted into the hydrochloride salt. 1(a)

In the subsequent PCT-international publication No. WO 02/02552 (glaxo) and its equivalent U.S. Pat. No. 7,157,466; the preparation of ditosylate salts of Lapatinib of formula-1(b) is disclosed as shown in Scheme-B.

In both of these patents, the process involves multiple steps to get the required product. The process is lengthy and cumbersome and also involves usage of corrosive chemicals like POCl3/SOCl2 etc.